Abstract:
:Lung cancer accounts for the highest death rate among cancers worldwide, with most patients being diagnosed with non-small cell lung cancer (NSCLC), urging more effective therapies. We report that JK273, a pyrrolo[2,3-d]pyrimidine analog, which inhibits α4 integrin signaling, showed a selective cytotoxic effect against HCI-H460 NSCLC cells, with an IC50 of 0.98 ± 0.15 μM, but showed less sensitivity to fibroblasts with a selectivity index (SI) greater than 30. This effect was attributed to cell cycle arrest at S phase by JK273 treatment, resulting in the apoptosis of NCI-H460 cells, further confirmed by exposing phosphatidylserine and morphological changes. Taken together with the previous study of JK273 inhibiting cell migration, we propose that JK273 could serve as an antitumor compound to specifically target cancer cells but not non-cancerous cells by triggering programmed cell death, in addition to anti-metastatic effects in cancer therapy.
journal_name
Biochem Biophys Res Communjournal_title
Biochemical and biophysical research communicationsauthors
Lu TN,Ganganna B,Pham TT,Vo AV,Lu TP,Nguyen HT,Nguyen MT,Huynh PN,Truong NT,Lee Jdoi
10.1016/j.bbrc.2017.07.096subject
Has Abstractpub_date
2017-09-16 00:00:00pages
355-360issue
2eissn
0006-291Xissn
1090-2104pii
S0006-291X(17)31446-8journal_volume
491pub_type
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